Table 2.
Cpd code | R | R’/Ar | MW | LogPa | Cytotoxicity (IC50,b μM)/Cell linesc |
||
---|---|---|---|---|---|---|---|
SW620 | PC3 | NCI-H23 | |||||
5b | -H | 2-Cl | 340.76 | 1.52 | 3.14 ± 0.56 | 3.99 ± 0.15 | 4.49 ± 0.24 |
5l | -H | 2,4-(OH)2 | 338.32 | 0.63 | 9.43 ± 0.27 | 16.52 ± 0.24 | 18.97 ± 3.43 |
5n | -H | 2-OH-4-OCH3 | 352.34 | 1.19 | 6.10 ± 0.68 | 8.46 ± 1.28 | 9.85 ± 1.28 |
5t | -Cl | 4-OCH3 | 370.79 | 1.60 | 2.45 ± 0.03 | 3.10 ± 0.32 | 3.34 ± 0.32 |
5u | -CH3 | -H | 320.35 | 1.42 | 3.52 ± 0.03 | 5.78 ± 0.06 | 9.77 ± 0.31 |
5x | -CH3 | 4-OCH3 | 350.37 | 1.50 | 4.99 ± 0.37 | 4.22 ± 0.63 | 4.05 ± 0.31 |
5z | -CH3 | 4-(NCH3)2 | 363.41 | 1.60 | 4.68 ± 0.30 | 4.60 ± 0.33 | 3.58 ± 0.11 |
7b | -I | -H | 473.22 | 1.21 | 3.97 ± 0.32 | 3.25 ± 0.15 | 2.81 ± 0.17 |
5-FUd | 130.08 | −0.81 | 8.84 ± 1.92 | 13.61 ± 0.46 | 13.45 ± 3.92 | ||
PAC-1 | 392.49 | 3.43 | 5.82 ± 0.20 | 4.16 ± 0.52 | 5.32 ± 0.21 |
aCalculated by EPI 320 software; bThe concentration (µM) of compounds that produces a 50% reduction in enzyme activity or cell growth, the numbers represent the averaged results from triplicate experiments with deviation of less than 10%.; cCell lines: SW620, colon cancer; PC3, prostate cancer; NCI-H23, lung cancer; d5-FU: 5-Fluorouracil, a positive control.